This invention relates to a composition of matter and method of using same which produces long lasting relief for patients suffering from a dry mouth condition.
Pilocarpine, as a free base, occurs as a colorless crystals with a melting point of 34.degree. C., and is soluble in water and ethyl alcohol. Pilocarpine and its nitrate and hydrochlorides salts, pilocarpine nitrate and pilocarpine hydrochloride, have long been known as parasympathetic alkaloids. Ingestion of pilocarpine or its salts causes stimulation of the GI track (reflected by an increase in GI motility) and stimulation of various glands, such as salivary glands, pancreas and mucosal cells in the respiratory track. Pilocarpine can also cause diaphoresis. Its internal administration may cause increased peristalsis of the intestines, intense bronchial spasms, accelerated heart and pulse rate, increased secretion by the stomach, increased bronchial secretions, and, if incautiously used, may cause pulmonary edema.
Pilocarpine has been used in internal medicine chiefly as a sudorific to evacuate dropsies or to eliminate toxic substances through the skin. It has been employed internally in the treatment of pruritus, to overcome the retention of urine which frequently occurs after pelvic operations and to induce sweating as a treatment for retrobulbar neuritis. When used as an internal medication it is generally administered as a hypodermic injection.
Today the principal use of pilocarpine is as a local remedy by opthalmologists as a myotic in a 0.5 to 8% solution for the treatment of glaucoma.
Furstenberg, Trans. Am. Laryng. Rhin. Otol. Soc., June 1944, pp. 48-54, disclosed that the oral administration of pilocarpine hydrochloride or pilocarpine nitrate in 10 milligram dosages three times a day temporarily restored salivation in patients suffering from dry mouth. It is apparent from Furstenberg that the remedial effect of the oral ingestion of pilocarpine alone is of very short duration. Thus, Furstenberg disclosed that to increase the longivity of the pilocarpine induced salivation, it is important to prepare the patient for maximum utilization and effectiveness of the drug. In the Furstenberg method the patient is placed in a mild state of acidosis by placing him on an alkali restricted diet and administering three grams of ammonium chloride with meals on a three-dayon and two-day-off basis. Such a diet caused an increase in the acidity of the body tissues which operated to extend the therapeutic action of the pilocarpine.
The Furstenberg method of treating dry mouth condition suffers from certain disadvantages in that: ingestion of pilocarpine may also produces undesirable systemic side effects such as increased sweating, constriction of the pupils, increased heart rate, increased secretion by the stomach, and increased bronchial secretions; and, to obtain prolonged relief the patient is required to follow a restricted diet.